PLX7904
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 206480

CAS#: 1393465-84-3

Description: PLX7904, also known as PB04, is a potent and selective paradox-breaker RAF inhibitor. PB04 is able to efficiently inhibit activation of ERK1/2 in mutant BRAF melanoma cells but does not hyperactivate ERK1/2 in mutant RAS-expressing cells. Importantly, PB04 inhibited ERK1/2 phosphorylation in mutant BRAF melanoma cells with acquired resistance to vemurafenib/PLX4720 that is mediated by a secondary mutation in NRAS. Consistent with ERK1/2 reactivation driving the re-acquisition of malignant properties, PB04 promoted apoptosis and inhibited entry into S phase and anchorage-independent growth in mutant N-RAS-mediated vemurafenib-resistant cells.


Chemical Structure

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PLX7904
CAS# 1393465-84-3

Theoretical Analysis

MedKoo Cat#: 206480
Name: PLX7904
CAS#: 1393465-84-3
Chemical Formula: C24H22F2N6O3S
Exact Mass: 512.14422
Molecular Weight: 512.54
Elemental Analysis: C, 56.24; H, 4.33; F, 7.41; N, 16.40; O, 9.36; S, 6.26

Size Price Shipping out time Quantity
10mg USD 90 Same day
25mg USD 150 Same day
50mg USD 250 Same day
100mg USD 450 Same day
200mg USD 750 Same day
500mg USD 1650 Same day
1g USD 2950 Same day
2g USD 5450 Same day
5g USD 8650 Same day
Inquire bulk and customized quantity

Pricing updated 2021-02-28. Prices are subject to change without notice.

PLX7904, purity > 98%, is in stock. The same day shipping out after order is received.

Synonym: PLX7904; PLX-7904; PLX 7904; PB04; PB-04; PB 04; paradox-breaker-04.

IUPAC/Chemical Name: 5-(2-Cyclopropylpyrimidin-5-yl)-3-[3-[[ethyl(methyl)sulfamoyl]amino]-2,6-difluorobenzoyl]-1H-pyrrolo[2,3-b]pyridine

InChi Key: DKNZQPXIIHLUHU-UHFFFAOYSA-N

InChi Code: InChI=1S/C24H22F2N6O3S/c1-3-32(2)36(34,35)31-19-7-6-18(25)20(21(19)26)22(33)17-12-30-24-16(17)8-14(9-29-24)15-10-27-23(28-11-15)13-4-5-13/h6-13,31H,3-5H2,1-2H3,(H,29,30)

SMILES Code: O=C(C1=CNC2=NC=C(C3=CN=C(C4CC4)N=C3)C=C21)C5=C(F)C=CC(NS(=O)(N(CC)C)=O)=C5F

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO, not in water

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code:
2934.99.9001

Preparing Stock Solutions

The following data is based on the product molecular weight 512.54 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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1: Zhang C, Spevak W, Zhang Y, Burton EA, Ma Y, Habets G, Zhang J, Lin J, Ewing T, Matusow B, Tsang G, Marimuthu A, Cho H, Wu G, Wang W, Fong D, Nguyen H, Shi S, Womack P, Nespi M, Shellooe R, Carias H, Powell B, Light E, Sanftner L, Walters J, Tsai J, West BL, Visor G, Rezaei H, Lin PS, Nolop K, Ibrahim PN, Hirth P, Bollag G. RAF inhibitors that evade paradoxical MAPK pathway activation. Nature. 2015 Oct 14. doi: 10.1038/nature14982. [Epub ahead of print] PubMed PMID: 26466569.

2: Basile KJ, Le K, Hartsough EJ, Aplin AE. Inhibition of mutant BRAF splice variant signaling by next-generation, selective RAF inhibitors. Pigment Cell Melanoma Res. 2014 May;27(3):479-84. doi: 10.1111/pcmr.12218. Epub 2014 Feb 10. PubMed PMID: 24422853; PubMed Central PMCID: PMC3988223.

3: Le K, Blomain ES, Rodeck U, Aplin AE. Selective RAF inhibitor impairs ERK1/2 phosphorylation and growth in mutant NRAS, vemurafenib-resistant melanoma cells. Pigment Cell Melanoma Res. 2013 Jul;26(4):509-17. doi: 10.1111/pcmr.12092. Epub 2013 Apr 8. PubMed PMID: 23490205; PubMed Central PMCID: PMC3695051.